Abstract: The invention relates to a method for determining the ability of a molecule to modulate the activation of a G protein-coupled receptor (GPCR), said method comprising the following steps: a) introducing, in a first container: a membrane preparation bearing one or more GPCRs and one or more alpha G-proteins, a source of nonhydrolyzable or slowly hydrolyzable GTP labeled with a first member of a pair of RET partners, a ligand of the alpha subunit of a G protein (alpha G-protein) labeled with a second member of the pair of RET partners, said ligand being capable of binding to the full alpha G-protein bound to the nonhydrolyzable or slowly hydrolyzable GTP labeled with the first member of a pair of RET partners, optionally a GPCR agonist; b) measuring the RET signal emitted in the first container; c) introducing (i) in a second container, the same reagents as in step a) and the molecule to be assayed or (ii) in the first container, the molecule to be assayed; d) measuring the RET signal emitted in the second

Abstract: The present invention relates to anti-metabotropic glutamate receptor subtype 2 (mGluR2) conformational single domain antibodies and uses thereof in particular in the therapeutic and diagnostic field.

Abstract: The present invention relates to anti-metabotropic glutamate receptor subtype 2 (mGluR2) conformational single do main antibodies and uses thereof in particular in the therapeutic and diagnostic field.

Abstract: The invention relates to hypophosphorous acid derivatives of formula (I) wherein —X is H or OH, —R represents one or several radicals R1-R5, identical or different, two of R1-R5 optionally occupying the same position on the phenyl group, one to four of R1-R5 being H and the others being selected in the group comprising -0-(CH2)n—COOH; —S—(CH2)n—COOH; —NH—(CH2)n—COOH; -0-(CH,R?)—COOH; —O—(CH2)n—OH; OR?, —R? being a C1-C3 alkyl radical; —OH; —COOH; halogen, particularly —F, —CI, —Br, —I, —CF3; —OCF3; —N02; —CH?CH—COOH; —(CH2)n—COOH; O—(CH2)n—P03H2; O—(CF2)n—P03H2; O—(CH2)n—S03H; O—(CH2)n—CONHOH; O—(CH2)n-tetrazol; O—(CH2)n-hydroxyisoxazol—n=1 to 5, preferably 1-3; said hypophosrous acid derivatives being diastereoisomers or enantiomers.

Abstract: The invention relates to hypophosphorous acid derivatives of formula (I) wherein —X is H or OH, —R represents one or several radicals R1-R5, identical or different, two of R1-R5 optionally occupying the same position on the phenyl group, one to four of R1-R5 being H and the others being selected in the group comprising -0-(CH2)n—COOH; —S—(CH2)n—COOH; —NH—(CH2)n—COOH; -0-(CH,R?)—COOH; —O—(CH2)n—OH; OR?, —R? being a C1-C3 alkyl radical; —OH; —COOH; halogen, particularly —F, —CI, —Br, —I, —CF3; —OCF3; —N02; —CH?CH—COOH; —(CH2)n—COOH; O—(CH2)n—P03H2; O—(CF2)n—P03H2; O—(CH2)n—S03H; O—(CH2)n—CONHOH; O—(CH2)n-tetrazol; O—(CH2)n-hydroxyisoxazol—n=1 to 5, preferably 1-3; said hypophosrous acid derivatives being diastereoisomers or enantiomers.

Abstract: The invention relates to a method for determining whether a test compound binds preferentially to a membrane receptor R1 or to a membrane receptor R2, these receptors being known to be expressed on the surface of the cells in monomeric, homodimeric or heterodimeric form. This method is applied using one or two FRET partner pairs.

Abstract: The invention relates to a method for determining whether a test compound binds preferentially to a membrane receptor R1 or to a membrane receptor R2, these receptors being known to be expressed on the surface of the cells in monomeric, homodimeric or heterodimeric form. This method is applied using one or two FRET partner pairs.

Abstract: The invention relates to the diastereoisomers of hypophosphorous acid derivatives, having formula (I), wherein the phenyl group is substituted by one or several atoms or groups, occupying one or several positions on the phenyl ring, and a method for the separation thereof.

Abstract: The invention relates to thiophosphi(o)nic acid derivatives having formula (I) wherein. M is a [C(R3,R4)]n1-C(E,COOR1,N(H,Z)) group, or an optionally substituted Ar—CH(COOR1,N(H,Z)) group (Ar designating an aryl or an heteroaryl group), or an ?, ? cyclic aminoacid group such as, formula (II) or a ?, &ggr;-cyclic aminoacid group such as, formula (III).

Abstract: A method for identifying and selecting a compound acting as an allosteric regulator of a GPCR-III is described. A method comparing the activity level of a recombinant GPCR-III (GPCR-III-?), essentially depleted of the extracellular domain of the corresponding native GPCR-III, in the presence of a given compound, with the activity level of the same GPCR-III-? is described. A method of identifying positive or negative allosteric regulators of GPCRs-III is described.

Abstract: Hypophosphorous acid derivatives having Formula (I) wherein .M is a [C(R3,R4)]n1-C(E,COOR1,N(H,Z)) group, or an optionally substituted Ar—CH(COOR1,N(H,Z)) group, or an a, ?, or a ?, g-cyclic amino acid; .R1 is H or R, R being an hydroxy or a carboxy protecting group; .Z is H or an amino protecting group R?, benzyl oxycarbonyl, benzyl or benzyl substituted; .E is H or a C1-C3 alkyl, aryl, an hydrophobic group; .

Abstract: The invention relates to a method for identifying and selecting a compound acting as an allosteric regulator of a GPCR-III. According to said method, the activity level of a recombinant GPCR-III (GPCR-III-?), essentially depleted of the extracellular domain of the corresponding native GPCR-III in the presence of a given compound, is compared to the activity level of the same GPCR-III? in the absence of said compound, enabling positive or negative allosteric regulators of GPCRs-III to be identified and selected. The invention also relates to the application of one such method for identifying and selecting compounds of interest in fields of activity such as pharmacy, the agro-food industry, the environment, ecology and basic research.

Abstract: The present invention relates to a method for the detection of ligands (agonists or antagonists) specific for a G protein-coupled receptor (GPCR), which comprises the steps consisting in: 1) bringing a receptor labelled with a member of a donor/acceptor pair into contact with a G? or G?? subunit of a G protein labelled with the other member of the donor/acceptor pair; 2) measuring the transfer by proximity effect between the donor and the acceptor.

Abstract: The invention concerns compounds of formula (I): in which: R1 to R4, identical or different, represent hydrogen, alkyl or aryl, themselves substituted if required, R1 and R2 together further capable of representing a bridge —(CH2)m in which m is a whole number from 1 to 5, or a bridge X representing a linear combination of m hydrocarbon groups, m being as defined above and comprising, if required, at least a heteroatom such as O, N or S, or a bridge X representing a linear combination of p heteroatoms O, N and/or S, in which p is a whole number from 1 to 3; A1 and A2 represent —COOH, —SO3H or —PO3H2 radicals, or their derivatives such as esters or amides, or only one of A1 or A2 has these meanings, when R1 and R2 represent a single bond between the carbons in positions 3 and 4, the other of these groups being a hydrogen atom; Y represents a chain —(CH2)n—, n being zero or a whole number from 1 to 5, or represents a linear combination of n hydrocarbon group